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The ProTide Prodrug Technology: From the Concept to the Clinic.

ABSTRACT: The ProTide technology is a prodrug approach developed for the efficient intracellular delivery of nucleoside analogue monophosphates and monophosphonates. In this approach, the hydroxyls of the monophosphate or monophosphonate groups are masked by an aromatic group and an amino acid ester moiety, which are enzymatically cleaved-off inside cells to release the free nucleoside monophosphate and monophosphonate species. Structurally, this represents the current end-point of an extensive medicinal chemistry endeavor that spans almost three decades. It started from the masking of nucleoside monophosphate and monophosphonate groups by simple alkyl groups and evolved into the sophisticated ProTide system as known today. This technology has been extensively employed in drug discovery, and it has already led to the discovery of two FDA-approved (antiviral) ProTides. In this work, we will review the development of the ProTide technology, its application in drug discovery, and its role in the improvement of drug delivery and efficacy.

SUBMITTER: Mehellou Y

PROVIDER: S-EPMC7075648 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature

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The ProTide Prodrug Technology: From the Concept to the Clinic.

Mehellou Youcef Y Rattan Hardeep S HS Balzarini Jan J

Journal of medicinal chemistry 20170824 6

The ProTide technology is a prodrug approach developed for the efficient intracellular delivery of nucleoside analogue monophosphates and monophosphonates. In this approach, the hydroxyls of the monophosphate or monophosphonate groups are masked by an aromatic group and an amino acid ester moiety, which are enzymatically cleaved-off inside cells to release the free nucleoside monophosphate and monophosphonate species. Structurally, this represents the current end-point of an extensive medicinal ...[more]

PMID: 28792763

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Project description:BackgroundCancer is a taxing chronic disease that demands substantial care, most of which is shouldered by informal caregivers. As a result, cancer caregivers often have to manage considerable challenges that could result in severe physical and psychological health consequences. Technology-based interventions have the potential to address many, if not all, of the obstacles caregivers encounter while caring for patients with cancer. However, although the application of technology-based interventions is on the rise, the term is seldom defined in research or practice. Considering that the lack of conceptual clarity of the term could compromise the effectiveness of technology-based interventions for cancer caregivers, timely research is needed to bridge this gap.ObjectiveThis study aims to clarify the meaning of technology-based interventions in the context of cancer caregiving and provide a definition that can be used by cancer caregivers, patients, clinicians, and researchers to facilitate evidence-based research and practice.MethodsThe 8-step concept analysis method by Walker and Avant was used to analyze the concept of technology-based interventions in the context of cancer caregiving. PubMed, PsycINFO, CINAHL, and Scopus were searched for studies that examined technology-based interventions for cancer caregivers.ResultsThe defining attributes of technology-based interventions were recognized as being accessible, affordable, convenient, and user-friendly. On the basis of insights gained on the defining attributes, antecedents to, and consequences of technology-based interventions through the concept analysis process, technology-based interventions were defined as the use of technology to design, develop, and deliver health promotion contents and strategies aimed at inducing or improving positive physical or psychological health outcomes in cancer caregivers.ConclusionsThis study clarified the meaning of technology-based interventions in the context of cancer caregiving and provided a clear definition that can be used by caregivers, patients, clinicians, and researchers to facilitate evidence-based oncology practice. A clear conceptualization of technology-based interventions lays foundations for better intervention design and research outcomes, which in turn have the potential to help health care professionals address the needs and preferences of cancer caregivers more cost-effectively.

Project description:ImportanceFatigue is a significant and debilitating symptom affecting 25% of the population. It occurs in those with a range of chronic diseases, can be idiopathic and in 0.2-0.4% of the UK population occurs in combination with other symptoms that together constitute chronic fatigue syndrome (CFS). Until recently, NHS clinical services only focussed upon CFS and excluded the majority of fatigued patients who did not meet the CFS diagnostic criteria. The CRESTA Fatigue interdisciplinary clinic was established in 2013 in response to this unmet need.ObjectiveTo identify the service needs of the heterogeneous group of patients accessing the CRESTA Fatigue Clinic, to prioritize these needs, to determine whether each is being met and to plan targeted service enhancements.DesignUsing a group concept mapping approach, we objectively identified the shared understanding of service users accessing this novel clinic.SettingNHS Clinics for Research & Service in Themed Assessment (CRESTA) Fatigue Clinic, Newcastle Upon Tyne, UK.ParticipantsPatients (n = 30) and referrers (n = 10) to the CRESTA Fatigue Clinic contributed towards a statement generation exercise to identify ways the clinic could support service users to improve their quality of life. Patients (n = 46) participated in the sorting and rating task where resulting statements were sorted into groups similar in meaning and rated for 'importance' and 'current success'.Main outcome and measureWe mapped the needs of patients attending the CRESTA Fatigue Clinic and identified which high-priority needs were being successfully met and which were not.ResultsMultidimensional scaling and hierarchical cluster analysis depicted the following eight themed clusters from the data which related to various service-user requirements: 'clinic ethos', 'communication', 'support to self-manage', 'peer support', 'allied health services', 'telemedicine', 'written information' and 'service operation'. Service improvement targets were identified within value bivariate plots of the statements.Conclusion and relevanceService development concepts were grouped into thematic clusters and prioritized for both importance and current success. The resulting concept maps depict where the CRESTA Fatigue Clinic successfully addresses issues which matter to patients and highlights areas for service enhancement. Unmet needs of patients have been identified in a rigorous service evaluation, and these are currently being addressed in collaboration with a service-user group.

Dataset Information

The ProTide Prodrug Technology: From the Concept to the Clinic.

Publications

The ProTide Prodrug Technology: From the Concept to the Clinic.

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